Paromomycin and neomycin B derived cationic lipids: Synthesis and transfection studies
Journal of Controlled Release. 2012-03-01; 158(3): 461-469
DOI: 10.1016/j.jconrel.2011.12.019
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1. J Control Release. 2012 Mar 28;158(3):461-9. doi: 10.1016/j.jconrel.2011.12.019.
Epub 2011 Dec 29.
Paromomycin and neomycin B derived cationic lipids: synthesis and transfection
studies.
Mével M(1), Sainlos M, Chatin B, Oudrhiri N, Hauchecorne M, Lambert O, Vigneron
JP, Lehn P, Pitard B, Lehn JM.
Author information:
(1)INSERM, U915, Nantes F-44000, France.
Cationic lipid-based nonviral gene delivery is an attractive approach for
therapeutic gene transfer. Basically, gene transfection can be achieved by using
synthetic vectors that compact DNA, forming cationic lipoplexes which can
interact with the cell plasma membrane by electrostatic interactions. Among the
basic components of any cationic lipid, the type of cationic headgroup has been
shown to have a major role in transfection efficiency. We have previously
reported the DNA transfection potential of vectors characterized by a kanamycin A
headgroup. The encouraging transfection results obtained with these compounds
prompted us to evaluate the potential of cationic lipids bearing headgroups based
on other aminoglycosides. Thus, we herein report the synthesis and gene
transfection properties of novel cationic lipids consisting of cholesteryl or
dioleyl moieties linked, via various spacers, to paromomycin or neomycin B
headgroups. Our results confirm that these new aminoglycoside-based cationic
lipids are efficient for gene transfection both in vitro and into the mouse
airways in vivo. We also investigated physico-chemical properties of the DNA
complexes formed by this particular type of synthetic vectors in order to better
understand their structure-activity relationships.
Copyright © 2011 Elsevier B.V. All rights reserved.
DOI: 10.1016/j.jconrel.2011.12.019
PMID: 22226775 [Indexed for MEDLINE]